CN104997795A - Applications of bigelovii A in preparing drugs used for preventing and treating inflammatory diseases - Google Patents
Applications of bigelovii A in preparing drugs used for preventing and treating inflammatory diseases Download PDFInfo
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- CN104997795A CN104997795A CN201510384427.0A CN201510384427A CN104997795A CN 104997795 A CN104997795 A CN 104997795A CN 201510384427 A CN201510384427 A CN 201510384427A CN 104997795 A CN104997795 A CN 104997795A
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- saponin
- bigelovii
- salicornia bigelovii
- bigelovii torr
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Abstract
The invention belongs to the field of natural drug, and relates to applications of specific monomer bigelovii A in Salicornia bigelovii Torr. in preparing drug compositions, and especially in preparing drug compositions used for preventing and treating inflammatory diseases. It is shown by in vitro inflammation model experiments that bigelovii A is capable of inhibiting generation of inflammatory induced prostaglandin E2 and release of nitric oxide; it is fond by in vivo experiments on animals that bigelovii A is capable of inhibiting phorbol ester induced mouse ear swelling; and it is confirmed by experiments that bigelovii A possesses obvious anti-inflammatory action on inflammatory diseases, and can be used for preparing drugs used for preventing and treating inflammatory diseases, wherein the inflammatory diseases include acute lung injury, rheumatic arthritis, inflammatory bowel disease, neurodegenerative disease, and septic shock.
Description
Technical field
The present invention relates to natural medicine field, be specifically related to the application of special monomer Salicornia Bigelovii Torr. saponin first (Bigelovii A) in pharmaceutical compositions in Salicornia bigelovii, the application especially in the pharmaceutical composition of preparation control inflammation related disease.
Background technology
Inflammatory reaction is one of important component part of body immune system, and body carries out accurate regulation and control by number of ways to it.But when inflammatory reaction is uncontrollable, body various diseases can be caused, as acute lung injury (acute lung injury), rheumatoid arthritis (rtheumatoid arthriti), inflammatory bowel (Inflammatory bowel disease, IBD), neurodegenerative disease (neurodegenerative disorder) and septic shock (septic shock syndrome) etc., long-term inflammatory reaction stimulates also can bring out body canceration (1, Zhu et al, Cancer Biol Ther, 2011, 12 (2): 95-105), these all serious threat the physical and mental health of people, therefore it is that the Main way of these disease medicaments is treated in exploitation at present that too drastic to body inflammatory reaction control effectively.Research shows, prostaglandin E
2(PGE
2), the inflammatory factor such as nitric oxide (NO) can be induced to express in inflammatory reaction, thus aggravation body degree of inflammation (2, Ricciotti E and FitzGerald GA, Arterioscler Thromb Vasc Biol, 2011,31 (5): 986-1000), therefore the inflammatory reaction by contributing to improving body is suppressed to these inflammatory factors.
Salicornia bigelovii, also known as than lucky Rockwell Salicornia Bigelovii Torr. (
salicornia bigeloviitorr.), for Chenopodiaceae salicornia europaeal belongs to annual stem carnification euhalophyte.The resistance to drought and waterlogging of Salicornia bigelovii, can plant at Coastal beach, salt-soda soil and lightweight sandy soil, and available sea water is directly irrigated or filled with fresh water is mixed, is particularly suitable for the growth of Subtropic of China Coastal beach area.Salicornia Bigelovii Torr. saponin first from Salicornia Bigelovii Torr. herb, is separated the one obtained fall pentacyclic triterpene saponin, and to human leukemia cell line HL-60 and human liver cancer cell HepG2, there is killing action, can be used for preparing antitumor drug (3, Dan Yu, number of patent application: 201110262116.9), but Salicornia Bigelovii Torr. saponin first to the effect of aspect of inflammation there are no report.
Summary of the invention
Salicornia Bigelovii Torr. saponin first is the object of the present invention is to provide to prepare the application of inflammation inhibitor, the application particularly in the diseases associated with inflammation medicine that mediated by inflammatory factor in preparation treatment endotoxin shock etc. of Salicornia Bigelovii Torr. saponin first.
From list of references [3], the chemical formula of described Salicornia Bigelovii Torr. saponin first is C
45h
70o
14, molecular weight is 834, and chemical structural formula is:
。
Described Salicornia Bigelovii Torr. saponin first can be used for preparing the diseases associated with inflammation medicine for the treatment of endotoxin shock etc. and being mediated by inflammatory factor.
Described diseases associated with inflammation comprises acute lung injury, rheumatic arthritis, inflammatory bowel, neurodegenerative disease, septic shock etc.
Salicornia Bigelovii Torr. saponin first can adopt prior art prepare or commercially availablely to obtain.
Through pharmacological evaluation confirm Salicornia Bigelovii Torr. saponin first can effectively the inflammation-inhibiting factor as prostaglandin E
2(PGE
2) and the expression of nitric oxide (NO); In addition, 20 mg/kg Salicornia Bigelovii Torr. saponin first have obvious inhibitory action to phorbol exters induced mice ear swelling, not worse than positive control Indomethacin effect.Can be used as the medicine of the diseases associated with inflammation that inflammation inhibitor is mediated by inflammatory factor for the preparation for the treatment of rheumatic arthritis, inflammatory bowel, neurodegenerative disease, septic shock etc.
The invention provides Salicornia Bigelovii Torr. saponin first and medically acceptable pharmaceutic adjuvant is prepared into pharmaceutical composition and preparation thereof.As, tablet, pill, unguentum, capsule, oral liquid, granule and injection injectable powder or liquid drugs injection liquid.
Accompanying drawing explanation
Can be used as APPENDIX MATERIALSThe with figure below to report.
The molecular structural formula of Fig. 1 Salicornia Bigelovii Torr. saponin first.
Fig. 2 Salicornia Bigelovii Torr. saponin first acts on the MTT experimental result picture after RAW264.7 cell.
Fig. 3 Salicornia Bigelovii Torr. saponin first suppresses prostaglandin E
2(PGE
2) effect.
#p<0.01 vs matched group;
*p<0.01 vs LPS processed group.
The effect of Fig. 4 Salicornia Bigelovii Torr. saponin first inflammation-inhibiting factor nitric oxide (NO).
#p<0.01 vs matched group;
*p<0.01 vs LPS processed group.
detailed description of the invention:
In conjunction with detailed description of the invention, the invention will be further described, but content of the present invention is not restricted to cited embodiment.
Embodiment 1 Salicornia Bigelovii Torr. saponin first cell toxicity test
Adopt MTT method to detect the cytotoxicity of Salicornia Bigelovii Torr. saponin first, concrete steps are as follows:
By RAW264.7 cell (2 × 10
5individual cells/well) access 96 well culture plate overnight incubation, add Salicornia Bigelovii Torr. saponin first (1,2,4,6,8, the 10 μ g/ml of variable concentrations, with DMSO as blank) combined effect 24h, then MTT to final concentration 0.5mg/ml effect 4h is added, DMSO is added by 100 μ l/ holes, shake 15 min, read absorbance at 570 nm wavelength places.
OD
570the growing state of cell can be reflected, according to OD
570calculate cell survival rate, thus judge whether Salicornia Bigelovii Torr. saponin first exists cytotoxicity.
MTT method testing result shows (see Fig. 2): Salicornia Bigelovii Torr. saponin first does not substantially have cytotoxicity to RAW264.7 cell under 1 ~ 10 μ g/ml concentration conditions.
Embodiment 2 Salicornia Bigelovii Torr. saponin first suppresses prostaglandin E
2(PGE
2) effect
The mouse macrophage RAW264.7 of trophophase of taking the logarithm spreads 24 orifice plates, attach overnight, adds Salicornia Bigelovii Torr. saponin first or positive control Indomethacin, adds the LPS process 24h of 100 ng/ml after 2h.Collecting cell culture fluid, 1000g, 15min, adopt the prostaglandin E in Inhibition ELISA detection supernatant
2.The results are shown in Figure 3.
Compared with the inflammatory model group of inducing with LPS, after giving Salicornia Bigelovii Torr. saponin first, the prostaglandin E that LPS inducing mouse macrophage RAW264.7 secretes
2obvious minimizing, and in good dose dependent.
Embodiment 3 Salicornia Bigelovii Torr. saponin first inflammation-inhibiting factor nitric oxide (NO) acts on
By RAW264.7 cell (1 × 10
6cell/mL) access 96 well culture plate overnight incubation, then Salicornia Bigelovii Torr. saponin first (0.1,1, the 10 μ g/ml of variable concentrations are added, with DMSO as blank), the LPS adding 100 ng/ml after 2h stimulates 24h, collecting cell culture supernatant, detects the content of nitric oxide (NO) by Griess method.
Experimental result (see Fig. 4) shows: Salicornia Bigelovii Torr. saponin first can nitric oxide production generation in the lipopolysaccharide-induced RAW264.7 cell of anti-bacteria, and in dose dependent.
The effect of embodiment 4 pairs of Mice Auricle phorbol exters inflammatory models
Healthy male ICR mouse 60, body weight 18 ~ 22g, is divided into following 5 groups at random, often organizes 12: (1) matched group, 0.5%CMC-Na, ig; (2) positive drug, indomethacin 20mg/kg, ig; (3) tested material high dose, 20mg/kg, ig; (4) dosage in tested material, 10mg/kg, ig; (5) tested material low dosage, 5mg/kg, ig.Adapted to raise through 5 days, each group mice overnight fasting before test.1 μ g phorbol exters is dissolved in 20 μ l acetone, is respectively coated with phorbol exters 10 μ l/ only for causing scorching ear in mouse right ear both sides, and it is non-ly cause scorching ear that left ear does not do any process.After causing scorching 0.5h, the corresponding test medicine of each group gavage.After administration 6h, dead 12 animals in every component other places, cut two ears, get circular auricle respectively, use scales/electronic balance weighing with the card punch of diameter 8mm from same area.Represent swelling with left and right auricle weight difference, the results are shown in Table 1.
Table 1 Salicornia Bigelovii Torr. saponin first is on the impact of phorbol exters induced mice ear swelling
(± S, n=12
)
| Group | Dosage (mg/kg) | Ear swelling degree (mg) | Suppression ratio (%) |
| Matched group | - | 19.6±2.47 | - |
| Indomethacin group | 20 | 9.5±1.26 * | 51.53 |
| Tested material low dosage | 5 | 13.53±1.26 * | 30.97 |
| Dosage in tested material | 10 | 11.48±1.75 * | 41.43 |
| Tested material high dose | 20 | 8.63±1.52 * | 55.97 |
Compare with matched group,
*p<0.01
Embodiment 5 is containing the tablet of Salicornia Bigelovii Torr. saponin first of the present invention
Get Salicornia Bigelovii Torr. saponin first 100 mg and starch 50 mg, dextrin 50 mg mixes, and makees wetting agent, make soft material with appropriate 30% ethanol, and conventional method is granulated, and adds the mixing of appropriate magnesium stearate, makes tablet.
Embodiment 6 is containing the capsule of Salicornia Bigelovii Torr. saponin first of the present invention
Get Salicornia Bigelovii Torr. saponin first 50 mg and starch 70 mg, dextrin 10 mg, Icing Sugar 10 mg mixes, and makees wetting agent, make soft material with appropriate 30% ethanol, and conventional method is granulated, and loads in hard capsule.
Embodiment 7 is containing the slow releasing capsule of Salicornia Bigelovii Torr. saponin first of the present invention
Get Salicornia Bigelovii Torr. saponin first 80mg and hydroxypropyl emthylcellulose K15M 120 mg, ethyl cellulose 45cps 40 mg, lactose 40 mg mix, appropriate with 10% vinylpyrrolidone k30 alcoholic solution, make soft material, conventional method is granulated, and loads in hard capsule and makes slow releasing capsule.
Claims (4)
1. one kind is fallen triterpene saponin componds Salicornia Bigelovii Torr. saponin first, it is characterized in that chemistry is by name: 3-O-(6 '-O-butyl)-β-D-pyranose aldehydic acid base-30-nor--12,20 (29)-diene oleanolic acid-28-O-β-D-glucopyranosyl esters, chemical structural formula is:
。
2. the Salicornia Bigelovii Torr. saponin first described in claim 1 is preparing the application of inflammation inhibitor, it is characterized in that described inflammation comprises acute pneumonia, rheumatic arthritis, inflammatory bowel, neurodegenerative disease or septic shock.
3. the pharmaceutical preparation that is prepared into of Salicornia Bigelovii Torr. saponin first according to claim 1 and medically acceptable pharmaceutic adjuvant.
4. pharmaceutical preparation as claimed in claim 3, it is characterized by dosage form is tablet, capsule, oral liquid, granule and lyophilized injectable powder.
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510384427.0A CN104997795B (en) | 2015-07-04 | 2015-07-04 | Purposes of the glasswort saponin(e first in preventing and treating inflammation related disease medicine is prepared |
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|---|---|---|---|
| CN201510384427.0A CN104997795B (en) | 2015-07-04 | 2015-07-04 | Purposes of the glasswort saponin(e first in preventing and treating inflammation related disease medicine is prepared |
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Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102408464A (en) * | 2011-09-06 | 2012-04-11 | 江苏省中国科学院植物研究所 | Novel notriterpenoid saponin compound and preparation method and application thereof |
-
2015
- 2015-07-04 CN CN201510384427.0A patent/CN104997795B/en active Active
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102408464A (en) * | 2011-09-06 | 2012-04-11 | 江苏省中国科学院植物研究所 | Novel notriterpenoid saponin compound and preparation method and application thereof |
Non-Patent Citations (1)
| Title |
|---|
| YOU AH KIM ETAL: "Evaluation of Salicornia herbacea as a Potential Anti oxidant and Anti-inflammatory agent", 《JOURNAL OF MEDICINAL FOOD》 * |
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